Compound for treating sequelae of ischemic cerebral stroke
a technology of ischemic cerebral stroke and compound, which is applied in the direction of peptides/proteins, drug compositions, peptides, etc., can solve the problems of increasing the burden of disease, affecting the health of middle-aged and elderly people in china, and the inability to meet the metabolic requirement of local cerebral tissues by the available blood supply,
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example 1
on of the Compound of Formula (III)
1. Solid Phase Synthesis of Peptide Chain
[0066]100 g of dichloro-tritylchloride resin (having a degree of substitution, of 1 mmol / g resin) was added into a 5 L reaction flask, to which 1 L dichloromethane was added. After 10 minutes, the resin sufficiently swelled in the solution, and 31.08 g of Fmoc-Tyr(tBu)—OH were added followed by 38 ml of DIEA. The reaction was continued for 30 minutes. Then, 1500 ml of methanol was added to terminate the reaction. The resin was filtered off, washed successively with isopropanol (IPA), DMF, isopropanol, DMF, isopropanol and ethyl ether, and dried in a fume hood to constant weight.
[0067]100 g of dried resin carrying Fmoc-Tyr(tBu)—OH was added into a 2 L reaction flask, and 1 L of DMF was added so that the resin sufficiently swelled in the solvent of DMF. DMF was drawn under a negative pressure into a waste liquid bottle, and 1 L of piperidine / DMF solution (25%) was added. The reaction flask was placed on a shak...
example 2
[0084]Normal male SD rats, weighing 280-320 g, were used in six experiments on 1.5-hour ischemia / reperfusion model groups (I1.5R+ model). Monitoring the scores of neuroethology symptoms 24 hours after the cerebral ischemia reperfusion injury and at each subsequent week in rats of the 1.5-hours ischemia / reperfusion model groups. The final results and sample size: results from the I1.5R+ model group in six experiments were combined (animal data: 31 animals in total in the I1.5R+model groups. In addition, the data of first week was the combined data from the experimental groups and the model group, the animal number in the 24-hour data was 101, and the animal number in the first week, data was 106).
[0085]The weights and scores of SD rats in the 1.5-hour ischemia / reperfusion model were recorded at 1.0 different time points later. The results showed that the weights of SD rats in the 1.5-hour ischemia / reperfusion showed a tendency of gradually rising, and the neurological score of 24-hou...
example 3
[0086]Normal male SD rats, weighing 280-320 g, were used in three experiments. In the first experiment, animals were divided randomly into two groups, one group in which the administration started one week after the 1.5-hour ischemia / reperfusion and continued for four weeks (I1.5R+1 week+dosing for 4 weeks), and the other group for the 1.5-hour ischemia / reperfusion model without administering, the compound of formula (III) (I1.5R+model). In the second experiment, animals were divided randomly into two groups, one group in which the administration started two weeks after the 1.5-hour ischemia / reperfusion and continued for four weeks (I1.5R+2 weeks+dosing for 4 weeks), and the other group for the 1.5-hour ischemia / reperfusion model without administering, the compound of formula (III) (I1.5R+model).
[0087]In the third experiment, animals were divided randomly into two groups, one group in which the administration started three days after the 1.5-hour ischemia / reperfusion and continued f...
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